Satzinger G
Gödecke AG, Forschung und Entwicklung, Freiburg, Fed. Rep. of Germany.
Arzneimittelforschung. 1994 Mar;44(3):261-6.
The importance of GABAergic neurons as the control sites at the central excitation level is generally accepted. Recently, knowledge has expanded concerning the participation of the GABAergic system in the pathophysiology of neurological and psychiatric diseases. Especially the pathogenesis of epilepsy is seen in connection with a loss of neuronal inhibitory function. Investigations into the structure and biochemistry of the central inhibitory transmitter GABA (gamma-aminobutyric acid) and the GABAA receptor resulted in medicinal-chemical strategies to stimulate GABAergic neurotransmission. With the synthesis of the GABA derivatives progabide, vigabatrin and gabapentin, a very promising enrichment of antiepileptic pharmacotherapy has become available.
γ-氨基丁酸能神经元作为中枢兴奋水平的控制位点的重要性已得到普遍认可。最近，关于γ-氨基丁酸能系统参与神经和精神疾病病理生理学的知识有所扩展。特别是癫痫的发病机制被认为与神经元抑制功能丧失有关。对中枢抑制性递质γ-氨基丁酸（GABA）和GABAA受体的结构与生物化学的研究产生了刺激γ-氨基丁酸能神经传递的药物化学策略。随着γ-氨基丁酸衍生物普罗加比、氨己烯酸和加巴喷丁的合成，抗癫痫药物治疗有了非常有前景的丰富成果。
